The growing understanding of the uses, safety, and therapeutic interventions of plant bioactives has led to the emergence of the latter, in synchronous amalgamation with contemporary systems of medicine. Various reports on chemoprotective action of plant bioactives has been increasing by 7%–15% per year and furnish new hope of light for scientists and researchers working in the domain of cancer. Phytobioactives, being derived from plants, comprise natural ingredients and, in this context, face only a few physicochemical challenges while being absorbed into the body. Further, these are readily metabolized by the body, thus producing fewer and milder side effects. This has augmented research in the development of various novel, nanostructured drug-delivery systems, considering plant bioactives as the prime focus. The present chapter highlights the various developments made in the field of plant bioactives, particularly their nanocarrier systems along with their potential uses.